TAK-683 acetate;
TAK-683 acetate 是一种有效的完全 KISS1R 激动剂 (IC50=170 pM)，具有改善的代谢稳定性。TAK-683 acetate 是一个九肽 metastin 的类似物，针对人与大鼠 EC50 值分别为 0.96 nM 和 1.6 nM。TAK-683 acetate 消耗下丘脑 GnRH，降低血浆 FSH、LH、睾酮水平，具有研究激素依赖性前列腺癌的潜力。
TAK-683 acetate Chemical Structure
| 规格 | 价格 | 是否有货 | 数量 |
|---|---|---|---|
| 1 mg | ￥3500 | In-stock | |
| 5 mg | ￥8500 | In-stock | |
| 10 mg | ￥14500 | In-stock | |
| 50 mg | ; | 询价 | ; |
| 100 mg | ; | 询价 | ; |
* Please select Quantity before adding items.
TAK-683 acetate 相关产品
bull;相关化合物库:
- Bioactive Compound Library Plus
- Peptide Library
| 生物活性 |
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][4]. |
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| 体外研究 (In Vitro) |
TAK-683 acetate exhibits an IC50 value (95% CI) from receptor binding assays is 150-180 pM and EC50 value (95% CI) from Ca+ mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 体内研究 (In Vivo) |
TAK-683 acetate (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced[3].TAK-683 acetate (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer[3].TAK-683 acetate (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
1358.50 |
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| Formula |
C66H87N17O15 |
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| Sequence Shortening |
N-Acetyl-YWNTF{aza}L{Met-R}W-NH2 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Protect from light, stored under nitrogen
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen) |
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| 溶解性数据 |
In Vitro:;
H2O : 5 mg/mL (3.68 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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| 参考文献 |
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